Sürdürülebilir Kalkınma Amaçları

• 1

Yazarlar

• Şahin, Engin(2)
• Can, Zehra(1)
• Cebeci, Fatma(1)
• Demirci, Yasin(1)
• Güler, Halil İbrahim(1)
• Izgi, Samet(1)
• Kalay, Erbay(1)
• Kandemir, Hakan(1)
• Kara, Yakup(1)
• Koca, Mehmet Serdar(1)
• Sengul, Ibrahim F.(1)

• MakaleAçık Erişim2023Scopus SJRQ3/r/bayburt/11849
  Synthesis of Arylsulfonyl Hydrazone Derivatives: Antioxidant Activity, Acetylcholinesterase Inhibition Properties, and Molecular Docking Study

  Demirci, Yasin; Kalay, Erbay; Kara, Yakup; Güler, Halil İbrahim; Can, Zehra; Şahin, Engin

  In this current paper, fifteen novel sulfonyl hydrazone derivatives have been successfully synthesized and evaluated for antioxidant activity as well as their effects on inhibitory activity toward acetylcholinesterase (AChE). By using 1H NMR, 13C NMR, FT-IR, and high-resolution mass spectrometry methods, the full characterization data of the novel compounds were obtained. The synthesized compounds capacity to inhibition glucosidase and exhibit antioxidant activity were tested in vitro. It was determined that compounds (E)-4-((2-((4-chlorophenyl)sulfonyl)hydrazone)methyl)-2-methoxyphenylfuran-2-carboxylate (21), (E)-2-methoxy-4-((2-(phenylsulfonyl)hydrazone)methyl)phenylfuran-2-carboxylate (17) and (E)-4-((2-((4-bromophenyl)sulfonyl)hydrazone)methyl)-2-methoxyphenylfuran-2-carboxylate (25) showed good antioxidant activity. Upon examining the acetylcholinesterase inhibitory activity, it was determined that compounds (E)-2-methoxy-4-((2-((4-methoxyphenyl)sulfonyl) hydrazone)methyl)phenylacetate (27) (10.39 μM), (E)-4-((2-((4-chloro phenyl)sulfonyl) hydrazone)methyl)-2-methoxyphenylfuran-2-carboxylate (21) (10.81 μM), (E)-4-((2-((4-chloro phenyl)sulfonyl)hydrazone)methyl)-2-methoxyphenyl thiophene-2-carboxylate (22) (12.92 μM) and (E)-2-methoxy-4-((2-(phenylsulfonyl)hydrazone)methyl)phenylfuran-2-carboxylate (17) (12.93 μM) showed potent inhibitory effects. Molecular docking simulations were used to investigate the interactions of novel sulfonyl hydrazone derivatives with human acetylcholinesterase protein. The ligands exhibited strong binding to the receptor protein with potent inhibition.

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  AtıfScopus18·WoS18·OpenAlex19

  İncele
• MakaleYalnız künye2022Scopus SJRQ2/r/bayburt/13339
  Synthesis of 7-azaindole based carbohydrazides and 1,3,4-oxadiazoles; Antioxidant activity, α-glucosidase inhibition properties and docking study

  Izgi, Samet; Sengul, Ibrahim F.; Şahin, Engin; Koca, Mehmet Serdar; Cebeci, Fatma; Kandemir, Hakan

  In this current work, 7-azaindole based 1,3,4-oxadiazoles have been successfully prepared by treatment of 3-(hydrazonomethyl)-7-azaindole with the different acyl chlorides or acetic anhydrides to give the corresponding carbohydrazides, followed by iodine mediated synthetic protocol in order to afford the corresponding 2,5-disubstituted 1,3,4-oxadiazoles. The full characterization data of the novel compounds were obtained by utilizing 1H NMR, 13C NMR, FT-IR, high-resolution mass spectrometry and single crystal X-ray diffraction techniques. The antioxidant activity and α-glucosidase inhibition potential of the prepared compounds are examined by in vitro assays. The targeted hydrazide linked 7-azaindoles and their corresponding cyclized form 1,3,4-oxadiazoles exhibited inhibitory potential with IC50 values ranges between 0.46 and 24.92 mM. Plausible binding mode and interaction of ligands with α-glucosidase enzyme have been studied by molecular docking, supporting the experimental results.

  AtıfScopus28·WoS27

  İncele